Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs.

The pentafluorosulfane (SF ₅ ) group, as a more electronegative bioisostere than the trifluoromethyl (CF ₃ ) group, has been gaining greater attention and increasingly reported usage in medicinal chemistry. Ostarine is the selective androgen receptor modulators (SARMs) containing a CF ₃ group in clinical trial III. In this study, 21 ostarine derivatives for replacing the CF ₃ group with SF ₅ substituents were synthesized. Some SF ₅ -derivatives showed androgen receptor (AR) agonistic activities in vitro. The results pointed to the potential of using this scaffold to develop new AR agonists.